83558-10-5Relevant academic research and scientific papers
Design and synthesis of phenoxymethybenzoimidazole incorporating different aryl thiazole-triazole acetamide derivatives as α-glycosidase inhibitors
Nasli Esfahani, Anita,Iraji, Aida,Alamir, Amir,Moradi, Shahram,Asgari, Mohammad Sadegh,Hosseini, Samanesadat,Mojtabavi, Somayeh,Nasli-Esfahani, Ensieh,Faramarzi, Mohammad Ali,Bandarian, Fatemeh,Larijani, Bagher,Hamedifar, Haleh,Hajimiri, Mir Hamed,Mahdavi, Mohammad
, (2021/09/18)
A novel series of phenoxymethybenzoimidazole derivatives (9a-n) were rationally designed, synthesized, and evaluated for their α-glycosidase inhibitory activity. All tested compounds displayed promising α-glycosidase inhibitory potential with IC50 values in the range of 6.31 to 49.89?μM compared to standard drug acarbose (IC50 = 750.0 ± 10.0?μM). Enzyme kinetic studies on 9c, 9g, and 9m as the most potent compounds revealed that these compounds were uncompetitive inhibitors into α-glycosidase. Docking studies confirmed the important role of benzoimidazole and triazole rings of the synthesized compounds to fit properly into the α-glycosidase active site. This study showed that this scaffold can be considered as a highly potent α-glycosidase inhibitor.
